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顺二氨二氯铂(II)快速输注、3小时输注和24小时输注后游离铂物种的药代动力学及其治疗意义。

Pharmacokinetics of free platinum species following rapid, 3-hr and 24-hr infusions of cis-diamminedichloroplatinum (II) and its therapeutic implications.

作者信息

Vermorken J B, van der Vijgh W J, Klein I, Gall H E, Pinedo H M

出版信息

Eur J Cancer Clin Oncol. 1982 Nov;18(11):1069-74. doi: 10.1016/0277-5379(82)90085-2.

DOI:10.1016/0277-5379(82)90085-2
PMID:6891650
Abstract

The pharmacokinetics of free platinum species derived from cis-diamminedichloroplatinum (II) (cisplatin) was studied in three patients who received the drug as a single agent for the first time at equal doses (100 mg/m2) but with different infusion times. In rapid, 3-hr and 24-hr infusions, peak levels of free platinum were 8.62, 1.96 and 0.27 microgram Pt/ml respectively; half-lives of disposition calculated 0-30 min after the end of each infusion were 17.4, 22.7 and 26.2 min respectively. Free platinum availability, measured as the area under the curves of the free platinum concentration, was the same for the three modes of administration (290, 321 and 325 micrograms Pt/min/ml-1 respectively). This observation supports the clinical impression that antitumour activity of cisplatin is not dependent on the method of administration.

摘要

对3例首次接受顺二氯二氨铂(顺铂)单药治疗的患者进行了研究,他们接受相同剂量(100mg/m²)但输注时间不同的顺铂治疗。在快速输注、3小时输注和24小时输注中,游离铂的峰值水平分别为8.62、1.96和0.27微克铂/毫升;每次输注结束后0至30分钟计算的处置半衰期分别为17.4、22.7和26.2分钟。以游离铂浓度曲线下面积衡量的游离铂可用性,三种给药方式相同(分别为290、321和325微克铂/分钟/毫升⁻¹)。这一观察结果支持了顺铂的抗肿瘤活性不依赖于给药方法的临床印象。

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